U.S. patent application number 10/218777 was filed with the patent office on 2003-01-02 for stable dentifrice compositions comprising polyphosphate, fluoride, and stannous.
This patent application is currently assigned to The Procter & Gamble Company. Invention is credited to Li, Baoan, Li, Yujun, Mao, Hsiang-Kuen, Mitra, Sekhar, Yue, Jiang.
Application Number | 20030003061 10/218777 |
Document ID | / |
Family ID | 22696252 |
Filed Date | 2003-01-02 |
United States Patent
Application |
20030003061 |
Kind Code |
A1 |
Yue, Jiang ; et al. |
January 2, 2003 |
Stable dentifrice compositions comprising polyphosphate, fluoride,
and stannous
Abstract
Disclosed are oral compositions comprising: (a) an effective
amount of one or more linear polyphosphates having an average chain
length of about 4 or more; (b) from about 0.15% to about 5% of a
fluoride ion source; (c) from about 0.1% to about 15% of a stannous
ion source; (d) an effective amount of a buffering agent; (e) from
about 6% to about 70% of an abrasive polishing material containing
less than 23% calcium; and (f) from about 40% to about 99% of one
or more aqueous carriers; wherein the oral composition has a total
water content of from about 1% to about 20%.
Inventors: |
Yue, Jiang; (West Chester,
OH) ; Mitra, Sekhar; (Guangzhou, CN) ; Li,
Yujun; (Kobe, JP) ; Mao, Hsiang-Kuen; (Kobe,
JP) ; Li, Baoan; (Guangzhou, CN) |
Correspondence
Address: |
THE PROCTER & GAMBLE COMPANY
INTELLECTUAL PROPERTY DIVISION
WINTON HILL TECHNICAL CENTER - BOX 161
6110 CENTER HILL AVENUE
CINCINNATI
OH
45224
US
|
Assignee: |
The Procter & Gamble
Company
Atten: Chief patent counsel 6090 center Hill Road
Cincinnati
OH
|
Family ID: |
22696252 |
Appl. No.: |
10/218777 |
Filed: |
August 14, 2002 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
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10218777 |
Aug 14, 2002 |
|
|
|
PCT/US01/07695 |
Mar 12, 2001 |
|
|
|
60189178 |
Mar 14, 2000 |
|
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|
Current U.S.
Class: |
424/52 ;
424/57 |
Current CPC
Class: |
A61K 8/25 20130101; A61K
8/18 20130101; A61K 8/24 20130101; A61K 8/21 20130101; A61Q 11/00
20130101 |
Class at
Publication: |
424/52 ;
424/57 |
International
Class: |
A61K 007/18; A61K
007/16 |
Claims
What is claimed is:
1. An oral composition comprising: a. an effective amount of one or
more linear polyphosphates having an average chain length of about
4 or more; b. from about 0.15% to about 5% of a fluoride ion
source; c. from about 0.1% to about 15% of a stannous ion source;
d. an effective amount of a buffering agent; e. from about 6% to
about 70% of an abrasive polishing material containing less than
23% calcium; and f. from about 50% to about 99% of one or more
aqueous carriers; wherein the oral composition has a total water
content of from about 1% to about 20%.
2. The oral composition according to claim 1 wherein the one or
more polyphosphates have an average chain length of 6 or more.
3. The oral composition according to claim 2 wherein each of the
one or more polyphosphates is present in an amount of from about
0.5% to about 30%.
4. The oral composition according to claim 3 wherein each of the
one or more polyphosphates is selected from the group consisting of
linear "glassy" polyphosphates having the formula
XO(XPO.sub.3).sub.nX wherein X is lithium, magnesium, sodium,
potassium, or ammonium and n averages from about 6 to about 21.
5. The oral composition according to claim 1 wherein the fluoride
ion source is sodium fluoride.
6. The oral composition according to claim 1 wherein the stannous
ion source is selected from the group consisting of stannous
chloride, stannous chloride dihydrate, stannous fluoride, stannous
sulfate, and mixtures thereof.
7. The composition according to claim 1 wherein the abrasive
polishing material is selected from the group consisting of
silicas, aluminas, phosphates, orthophosphates, polymetaphosphates,
and mixtures thereof.
8. The oral composition according to claim 1 wherein the aqueous
carriers are materials selected from the group consisting of
humectants, peroxide sources, alkali metal bicarbonate salts,
surfactants, thickening materials, water, titanium dioxide, mica,
flavor systems, sweetening agents, xylitol, coloring agents, urea,
desensitising agents, and mixtures thereof.
9. The oral composition according to claim 1 wherein the humectant
is selected from the group consisting of glycerin, propylene
glycol, polyethylene glycol, and mixtures thereof.
10. The oral composition according to claim 1 wherein the
composition is a single-phased dentifrice composition.
11. The oral composition according to claim 10 wherein the oral
composition has a total water content of from about 2% to about
14%.
12. The oral composition according to claim 11 wherein the oral
composition has a total water content of from about 3% to about
10%.
13. A method for reducing the incidence of calculus on dental
enamel comprising contacting the enamel surfaces in the mouth with
the oral composition according to claim 1.
Description
CROSS REFERENCE RELATED TO APPLICATIONS
[0001] This is a continuation of International Application
PCT/US01/07695 with an international filing date of Mar. 12, 2001,
which claims benefit of Provisional Application Serial No.
60/189,178 filed Mar. 14, 2000.
SUMMARY OF THE INVENTION
[0002] The present invention relates to a stable oral composition
comprising polyphosphate, a fluoride ion source, and a stannous ion
source. More specifically, the present invention relates to a
single-phase such dentifrice composition.
BACKGROUND OF THE INVENTION
[0003] Dental calculus, or tartar as it is sometimes called, is a
deposit which forms on the surfaces of the teeth at the gingival
margin. Supragingival calculus appears principally in the areas
near the orifices of the salivary ducts; e.g., on the lingual
surfaces of the lower anterior teeth and on the buccal surfaces of
the upper first and second molars, and on the distal surfaces of
the posterior molars.
[0004] Mature calculus consists of an inorganic portion which is
largely calcium phosphate arranged in a hydroxyapatite crystal
lattice structure similar to bone, enamel, and dentine. An organic
portion is also present and consists of desquamated epithelial
cells, leukocytes, salivary sediment, food debris, and various
types of microorganisms.
[0005] As the mature calculus develops, it becomes visibly white or
yellowish in color unless stained or discolored by some extraneous
agent. This is undesirable from an aesthetic standpoint.
[0006] Mechanical removal of calculus periodically by the dentist
is routine dental office procedure. A variety of chemical and
biological agents have also been suggested to retard calculus
formation or to remove calculus after it is formed. Pyrophosphate
salts are chemical agents known to have the ability to retard
calculus formation as described, for example, in U.S. Pat. No.
4,999,184, to Parran, Jr. et al., issued Mar. 12, 1991.
[0007] In addition to the pyrophosphate salts, other polyphosphates
are also known to help retard calculus formation. U.S. Pat. No.
4,627,977, issued Dec. 9, 1986, to Gaffar et al. discloses the use
of linear molecularly dehydrated polyphosphate salts combined with
a fluoride ion-providing source and a synthetic linear polymeric
polycarboxylate which inhibit enzymatic hydrolysis of the
polyphosphate salt in saliva. U.S. Pat. No. 4,247,526, to Jarvis et
al., issued Jan. 27, 1981, discloses the use of a pharmaceutically
acceptable condensed phosphate salt in addition to dicalcium
phosphate dihydrate and trimagnesium phosphate. Although
polyphosphate containing oral care products are known, there is a
continuing need to develop stable products containing
polyphosphates.
[0008] Certain polyphosphates, in particular, linear polyphosphates
with average chain lengths greater than 4, will significantly react
with most ionic fluoride sources in oral compositions and alter the
pH of the oral compositions. This reaction compromises the ability
of the oral composition to provide stable ionic fluoride and
polyphosphate to the oral surfaces. It has been described that
sodium monofluorophosphate is a suitable fluoride ion source to be
present with polyphosphate in a single-phased dentifrice
composition, see WO 98/22080, published on May 28, 1998. However,
it remains desirable to have a wider range of soluble fluoride ion
source without compromising stability. Fluoride ion is, of course,
a well-known caries protection agent.
[0009] In addition, these polyphosphates are hydrolytically
unstable, as well as highly hygroscopic, i.e., they decompose very
rapidly in the presence of water. Thus, the use of expensive dual
compartment dispensers to keep the polyphosphate separated from the
aqueous components of the formulation until just prior to use is
generally necessary, to ensure product stability. This generally
increases the cost of the formulation to consumers; which to some
consumers, especially those in developing countries and/or those
with less access to professional dental office prophylaxis, may
make such products less desirable to consumers.
[0010] Stannous (II) ion has been found to help in the reduction of
gingivitis, plaque, sensitivity, and to provide improved breath
benefits. Polyphosphate can chelate with stannous ion in solution
such that the stringent taste of the stannous can greatly be
reduced. In addition, polyphosphates are effective in preventing
tin deposition on teeth which results in staining. However, like
polyphosphate, stannous (II) has a short life in solution, as it
converts from stannous (II) to stannous (IV) easily.
[0011] Therefore, there remains a need to provide oral
compositions, in particular single-phased oral compositions, in
which the polyphosphate and the stannous ions are stabilized, and
in which soluble fluoride ion can be efficaciously incorporated.
None of the existing art provides all of the advantages and
benefits of the present invention.
SUMMARY OF THE INVENTION
[0012] The present invention relates to an oral composition
comprising: (a) an effective amount of one or more linear
polyphosphates having an average chain length of about 4 or more;
(b) from about 0.15% to about 5% of a fluoride ion source; (c) from
about 0.1% to about 15% of a stannous ion source; (d) an effective
amount of a buffering agent; (e) from about 6% to about 70% of an
abrasive polishing material containing less than 23% calcium; and
(f) from about 40% to about 99% of one or more aqueous carriers;
wherein the oral composition has a total water content of from
about 1% to about 20%.
[0013] These and other features, aspects, and advantages of the
present invention will become evident to those of skill in the art
from a reading of the present disclosure.
DETAILED DESCRIPTION OF THE INVENTION
[0014] All percentages and ratios used herein are by weight of the
oral composition, unless otherwise specified. All measurements
referred to herein are made at 25.degree. C., unless otherwise
specified.
[0015] All percentages, ratios, and levels of ingredients referred
to herein are based on the actual amount of the ingredient, and do
not include solvents, fillers, or other materials with which the
ingredient may be combined as a commercially available product,
unless otherwise specified.
[0016] All publications, patent applications, and issued patents
referred to herein are incorporated herein by reference in their
entireties. Citation of any reference is not an admission regarding
any determination as to its availability as prior art to the
claimed invention.
[0017] Herein, "comprising" means that other steps and other
components which do not affect the end result can be added. This
term encompasses the terms "consisting of" and "consisting
essentially of."
[0018] Herein, "effective amount" means an amount of a compound of
composition sufficient to significantly induce a positive benefit,
preferably an oral health benefit, but low enough to avoid serious
side effects, i.e., to provide a reasonable benefit to risk ratio,
within the sound judgment of a skilled artisan.
[0019] The oral composition of the present invention may be in the
form of a toothpaste or dentifrice. The term "dentifrice", as used
herein, means paste, gel, or liquid formulations unless otherwise
specified. The dentifrice composition may be in any desired form,
such as deep striped, surface striped, multilayered, having the gel
surrounding the paste, or any combination thereof. Alternatively,
the oral composition may be one of the dentifrice compositions in a
dual phase system comprising two dentifrice compositions contained
in a physically separated compartment of a dispenser and dispensed
side-by-side.
[0020] The term "dispenser", as used herein, means any pump, tube,
or container suitable for dispensing toothpaste.
[0021] The term "oral composition" as used herein means the total
dentifrice that is delivered to the oral surfaces. The oral
composition is a product, which in the ordinary course of usage, is
not intentionally swallowed for purposes of systemic administration
of particular therapeutic agents, but is rather retained in the
oral cavity for a time sufficient to contact substantially all of
the dental surfaces and/or oral tissues for purposes of oral
activity.
[0022] The term "aqueous carrier" as used herein means any safe and
effective materials for use in the compositions of the present
invention. Such materials include abrasive polishing materials,
peroxide sources, alkali metal bicarbonate salts, thickening
materials, humectants, water, surfactants, titanium dioxide, mica,
flavor systems, sweetening agents, xylitol, coloring agents,
desensitizing agents, urea, and mixtures thereof.
[0023] The present compositions comprise essential components, as
well as optional components. The essential and optional components
of the compositions of the present invention are described in the
following paragraphs.
[0024] Polyphosphate Source
[0025] The present invention includes a polyphosphate source. A
polyphosphate is generally understood to consist of two or more
phosphate molecules arranged primarily in a linear configuration,
although some cyclic derivatives may be present. Although
pyrophosphates are a polyphosphate, the polyphosphates desired are
those having 4 or more phosphate molecules. The pyrophosphates are
discussed separately. The inorganic polyphosphate salts desired
include tetrapolyphosphate and hexametaphosphate, among others.
Polyphosphates larger than tetrapolyphosphate usually occur as
amorphous glassy materials. Preferred in this invention are the
linear "glassy" polyphosphates having the formula:
XO(XPO.sub.3).sub.nX
[0026] wherein X is lithium, magnesium, sodium, potassium, or
ammonium, preferably sodium or potassium, and n averages from about
6 to about 125. Preferred are polyphosphates manufactured by FMC
Corporation which are commercially known as Sodaphos (n.apprxeq.6),
Hexaphos (n.apprxeq.13), and Glass H (n.apprxeq.21). Such materials
are also available from, e.g., the Jiang Su Cheng Xing Chemical
Co., Jiang Yin City, Jiang Su province, China. These polyphosphates
may be used alone or in any combination thereof.
[0027] The phosphate sources are described in more detail in Kirk
& Othmer, Encycl. Chemical Technology, Fourth Edition, Volume
18, Wiley-Interscience Publishers (1996). The polyphosphate source
will typically comprise from about 0.5% to about 30%, preferably
from about 2% to about 26%, more preferably from about 3% to about
20%, and most preferably from about 4% to about 13%, by weight of
the oral composition.
[0028] Fluoride Ion Source
[0029] The dentifrice composition of the present invention
incorporates a soluble fluoride ion source capable of providing
free fluoride ions. Fluoride ion sources are well known for use in
oral compositions as anti-caries agents. Preferred soluble fluoride
ion sources herein include sodium fluoride, stannous fluoride,
indium fluoride, potassium fluoride, ammonium fluoride, sodium
monofluorophosphate, and mixtures thereof. Norris et al., U.S. Pat.
No. 2,946,725, issued Jul. 26, 1960, and Widder et al., U.S. Pat.
No. 3,678,154 issued Jul. 18, 1972, disclose such fluoride ion
sources as well as others. Sodium fluoride is a highly preferred
soluble fluoride ion source.
[0030] The present compositions may contain a soluble fluoride ion
source capable of providing from about 50 ppm to about 3500 ppm,
and preferably from about 500 ppm to about 3000 ppm of free
fluoride ions. To deliver the desired amount of fluoride ions,
fluoride ion sources may be present in the total oral composition
at an amount of from about 0.15% to about 5%, preferably from about
0.2% to about 1%, and more preferably from about 0.2% to about
0.6%, by weight of the total composition delivered to the oral
cavity.
[0031] Stannous Ion Source
[0032] The present composition includes a stannous ion source,
preferably a stannous (II) ion. Stannous has been found to help in
the reduction of gingivitis, plaque, sensitivity, and in improving
breath benefits. The stannous provided in an oral composition will
provide efficacy to a subject using the composition. Formulations
providing efficacy typically include stannous levels ranging from
about 3,000 ppm to about 15,000 ppm stannous ions in the
composition. Below 3,000 ppm stannous the efficacy of the stannous
is not sufficient. Preferably, the stannous ion is present in an
amount of about 4,000 ppm to about 12,000 ppm, more preferably
5,000 ppm to about 10,000 ppm. These are ranges of stannous ions
representative of a single phase oral composition. If the stannous
ions were in one phase of a dual phase composition, the stannous
concentration would be doubled.
[0033] Dentifrices containing stannous salts, particularly stannous
fluoride and stannous chloride, are described in U.S. Pat. No.
5,004,597 to Majeti et al. Other descriptions of stannous salts are
found in U.S. Pat. No. 5,578,293 issued to Prencipe et al. and in
U.S. Pat. No. 5,281,410 issued to Lukacovic et al. The stannous
ions herein are preferably provided from a stannous chloride,
stannous chloride dihydrate, stannous fluoride, stannous sulfate,
and/or other stannous salt that is added to the oral composition,
with stannous chloride, stannous chloride dihydrate, stannous
fluoride, stannous sulfate, and mixtures thereof being preferred.
In general, stannous chloride and stannous chloride dihydrate are
less costly sources of stannous as compared to stannous fluoride;
because they are believed to deliver equally efficacious benefits
as compared to stannous fluoride, they are preferred for use when
it is desirable to manage the overall cost of the composition.
[0034] Other desirable stannous salts include stannous acetate,
stannous gluconate, stannous oxalate, stannous lactate, and
stannous tartrate.
[0035] In addition to the stannous ion source, other ingredients
needed to stabilize the stannous may also be included, such as the
ingredients described in Majeti et al. and Prencipe et al.
[0036] The combined stannous salts will be present in an amount of
from about 0.1% to about 15%, by weight of the total composition.
Preferably, the stannous salts are present in an amount of from
about 0.5 to about 7%, more preferably from about 1% to about 5%,
and most preferably from about 1.5% to about 3% by weight of the
total composition.
[0037] Buffering Agent
[0038] The present composition contains a buffering agent.
Buffering agents, as used herein, refer to agents that can be used
to adjust the pH of the compositions to a range of about pH 6.5 to
about pH 10. These agents include alkali metal hydroxides,
carbonates, sesquicarbonates, borates, silicates, phosphates,
imidazole, and mixtures thereof. Specific buffering agents include
monosodium/monopotassium phosphate, disodium/dipotassium phosphate,
trisodium/tripotassium phosphate, sodium hydroxide, potassium
hydroxide, alkali metal carbonate salts, sodium carbonate,
imidazole, pyrophosphate salts, citric acid, and sodium/potassium
citrate. Buffering agents are used at a level of from about 0.1% to
about 30%, preferably from about 1% to about 10%, and more
preferably from about 0.5% to about 3%, by weight of the present
composition.
[0039] Pyrophosphate Salt
[0040] Pyrophosphate salts may also be buffering agents. The
pyrophosphate salts useful in the present compositions include the
dialkali metal pyrophosphate salts, tetra alkali metal
pyrophosphate salts, and mixtures thereof. Disodium dihydrogen
pyrophosphate (Na.sub.2H.sub.2P.sub.2O.sub.7- ), trisodium hydrogen
pyrophosphate (Na.sub.3HP.sub.2O.sub.7), tetrasodium pyrophosphate
(Na.sub.4P.sub.2O.sub.7), and tetrapotassium pyrophosphate
(K.sub.4P.sub.2O.sub.7) in their unhydrated as well as hydrated
forms are the preferred species. In compositions of the present
invention, the pyrophosphate salt may be present in one of three
ways: predominately dissolved, predominately undissolved, or a
mixture of dissolved and undissolved pyrophosphate.
[0041] Compositions comprising predominately dissolved
pyrophosphate refer to compositions where at least one
pyrophosphate ion source is in an amount sufficient to provide at
least about 1.0% free pyrophosphate ions. The amount of free
pyrophosphate ions may be from about 1% to about 15%, preferably
from about 1.5% to about 10%, and most preferably from about 2% to
about 6%, by weight of the composition. Free pyrophosphate ions may
be present in a variety of protonated states depending on a the pH
of the composition.
[0042] Compositions comprising predominately undissolved
pyrophosphate refer to compositions containing no more than about
20% of the total pyrophosphate salt dissolved in the composition,
preferably less than about 10% of the total pyrophosphate dissolved
in the composition. Tetrasodium pyrophosphate salt is the preferred
pyrophosphate salt in these compositions. Tetrasodium pyrophosphate
may be the anhydrous salt form or the decahydrate form, or any
other species stable in solid form in the dentifrice compositions.
The salt is in its solid particle form, which may be its
crystalline and/or amorphous state, with the particle size of the
salt preferably being small enough to be aesthetically acceptable
and readily soluble during use. The amount of pyrophosphate salt
useful in making these compositions is any tartar control effective
amount, and is generally from about 1.5% to about 15%, preferably
from about 2% to about 10%, and most preferably from about 2.5% to
about 8%, by weight of the composition. Some or all of the
tetrasodium pyrophosphate maybe undissolved in the product and
present as tetrasodium pyrophosphate particles. Pyrophosphate ions
in different protonated states (e.g., HP.sub.2O.sub.7.sup.-3) may
also exist depending upon the pH of the composition and if part of
the tetrasodium pyrophosphate is dissolved.
[0043] Compositions may also comprise a mixture of dissolved and
undissolved pyrophosphate salts. Any of the above mentioned
pyrophosphate salts may be used.
[0044] The pyrophosphate salts are described in more detail in Kirk
& Othmer, Encyclopedia of Chemical Technology, Third Edition,
Volume 17, Wiley-lnterscience Publishers (1982).
[0045] Optional agents to be used in place of or in combination
with the pyrophosphate salt include such materials known to be
effective in reducing calcium phosphate mineral deposition related
to calculus formation. Agents included are synthetic anionic
polymers [including polyacrylates and copolymers of maleic
anhydride or acid and methyl vinyl ether (e.g., Gantrez), as
described, for example, in U.S. Pat. No. 4,627,977, to Gaffar et
al.; as well as, e.g., polyamino propoane sulfonic acid (AMPS)],
zinc citrate trihydrate, diphosphonates (e.g., EHDP; AHP),
polypeptides (such as polyaspartic and polyglutamic acids), and
mixtures thereof.
[0046] Aqueous Carriers
[0047] In preparing the present compositions, it is desirable to
add one or more aqueous carriers to the compositions. Such
materials are well known in the art and are readily chosen by one
skilled in the art based on the physical and aesthetic properties
desired for the compositions being prepared. Aqueous carriers
typically comprise from about 40% to about 99%, preferably from
about 70% to about 98%, and more preferably from about 90% to about
95%, by weight of the oral composition.
[0048] Abrasive Polishing Materials
[0049] An abrasive polishing material is generally included in the
toothpaste compositions. The abrasive polishing material
contemplated for use in the compositions of the present invention
can be any material which does not excessively abrade dentin. The
abrasive polishing material must have a calcium content of less
than 23%. Without being limited by theory, it is believed that such
a calcium content is desirable to reduce interaction between the
fluoride ion source and incompatible materials present in the
abrasive polishing material, e.g., calcium. Typical abrasive
polishing materials include silicas including gels and
precipitates; aluminas; phosphates including orthophosphates,
polymetaphosphates, and pyrophosphates; and mixtures thereof.
Specific examples include dicalcium orthophosphate dihydrate,
calcium pyrophosphate, tricalcium phosphate, calcium
polymetaphosphate, insoluble sodium polymetaphosphate, hydrated
alumina, beta calcium pyrophosphate, calcium carbonate, and
resinous abrasive materials such as particulate condensation
products of urea and formaldehyde, and others such as disclosed by
Cooley et al in U.S. Pat. No. 3,070,510, issued Dec. 25, 1962.
Mixtures of abrasives may also be used. Only the abrasive polishing
materials containing less than 23% calcium may be used in a single
phase system herein.
[0050] Silica dental abrasives of various types are preferred
because of their unique benefits of exceptional dental cleaning and
polishing performance without unduly abrading tooth enamel or
dentine. The silica abrasive polishing materials herein, as well as
other abrasives, generally have an average particle size ranging
between about 0.1 to about 30 microns, and preferably from about 5
to about 15 microns. The abrasive can be precipitated silica or
silica gels such as the silica xerogels described in Pader et al.,
U.S. Pat. No. 3,538,230, issued Mar. 2, 1970, and DiGiulio, U.S.
Pat. No. 3,862,307, issued Jan. 21, 1975. Preferred are the silica
xerogels marketed under the trade name "Syloid" by the W. R. Grace
& Company, Davison Chemical Division. Also preferred are the
precipitated silica materials such as those marketed by the J. M.
Huber Corporation under the trade name, "Zeodent", particularly the
silica carrying the designation "Zeodent 119". The types of silica
dental abrasives useful in the toothpastes of the present invention
are described in more detail in Wason, U.S. Pat. No. 4,340,583,
issued Jul. 29, 1982. Silica abrasives are also described in U.S.
patent application Ser. Nos. 08/434,147 and 08/434,149, both filed
May 2, 1995. The abrasive in the toothpaste compositions described
herein is generally present at a level of from about 6% to about
70% by weight of the composition. Preferably, toothpastes contain
from about 10% to about 50% of abrasive, by weight of the oral
composition.
[0051] Humectant
[0052] Another preferred aqueous carrier desired herein is a
humectant. The humectant serves to keep toothpaste compositions
from hardening upon exposure to air and certain humectants can also
impart desirable sweetness of flavor to toothpaste compositions.
Suitable humectants for use in the invention include glycerin,
sorbitol, polyethylene glycol, propylene glycol, and other edible
polyhydric alcohols. The humectant generally comprises from about
0% to 70%, and preferably from about 15% to 55%, by weight of the
composition.
[0053] Herein, glycerin, polyethylene glycol, propylene glycol, and
mixtures thereof are the preferred humectants. It is known that the
polyphosophate and the stannous ion sources herein decompose in the
presence of water. It has been discovered that if the
polyphosophate and the stannous ion sources herein are dispersed in
the humectant during manufacture, the stability of these components
can be maintained in the product form. Since the overall amount of
water contained in the composition is low, i.e., from about 1% to
about 20%, preferably from about 2% to about 14%, and more
preferably from about 3% to about 10%, dispersing both the
polyphosphate and the stannous source in the matrix ensures the
stability of each of these two components.
[0054] As used herein, "stable" refers to the amount of total
soluble fluoride content, the amount of total soluble stannous
content, and the amount of released orthophosphate from the
polyphosphate hydrolysis of the composition. To determine if the
composition is stable, the total soluble fluoride and total soluble
stannous present in the composition may be measured by methods
known to those of skill in the art. If there is a significant loss
of soluble fluoride and/or soluble stannous, the composition is not
stable.
[0055] The amount of orthophosphate can be measured, e.g., using
31P-NMR method. If the amount of orthophosphate is not
significantly increased over a certain period at a certain
temperature, the polyphosphate is stable. For example, it is
believed that the level of orthophosphate released as a result of
polyphosphate hydrolysis in the compositions herein is not greater
than 2% after 3 months at room temperature.
[0056] Additionally, the appearance of a white precipitate may also
be a measure of stability. Appearance of a white precipitate
indicates that the composition is not stable. Without being limited
by theory, it is believed that the compositions herein will exhibit
stability during ordinary storage and shelf life conditions of time
and temperature.
[0057] In this manner, an efficacious, stable, and single-phased
dentifrice composition can be provided. Because there is no need to
keep those components that decompose in water separated from those
that are stable in water until just prior to use, such a
composition need not be dispensed from a dual compartment
dispenser. Thus, the composition can efficaciously deliver oral
care actives without increasing the cost associated with
packaging.
[0058] This being said however, it should be understood that the
present invention is not limited to a single-phased composition.
The present invention includes dual-phased compositions in which
two oral formulations are contained in physically separate
compartments of a dentifrice dispenser. In general, the
polyphosphate should be separated from the fluoride and stannous
ion sources. By way of example, one of the two oral formulations
comprises the polyphosphate, the stannous ion source, an effective
amount of a buffering agent, and one or more aqueous carriers, the
total water content being from about 1% to about 20%, preferably
from about 2% to about 14%, and more preferably from about 3% to
about 10%; and the other oral formulation generally comprises the
fluoride ion source, an effective amount of a buffering agent, and
one or more aqueous carriers; the total water content being from
about 1% to about 20%.
[0059] Peroxide Source
[0060] The present compositions may include a peroxide source. The
peroxide source is preferably selected from the group consisting of
hydrogen peroxide, calcium peroxide, urea peroxide, and mixtures
thereof. The following amounts represent the amount of peroxide raw
material, although the peroxide source may contain ingredients
other than the peroxide raw material. The present composition may
contain from about 0.01 % to about 10%, preferably from about 0.1%
to about 5%, more preferably from about 0.2% to about 3%, and most
preferably from about 0.3% to about 0.8% of a peroxide source, by
weight of the dentifrice composition.
[0061] Alkali Metal Bicarbonate Salt
[0062] The present invention may also include an alkali metal
bicarbonate salt. Alkali metal bicarbonate salts are soluble in
water and unless stabilized, tend to release carbon dioxide in an
aqueous system. Sodium bicarbonate, also known as baking soda, is
the preferred alkali metal bicarbonate salt. The alkali metal
bicarbonate salt also functions as a buffering agent. The present
composition may contain from about 0.5% to about 50%, preferably
from about 0.5% to about 30%, more preferably from about 2% to
about 20%, and most preferably from about 5% to about 18% of an
alkali metal bicarbonate salt, by weight of the oral
composition.
[0063] Additional Aqueous Carriers
[0064] The present invention compositions in the form of
toothpastes, typically contain some thickening material or binders
to provide a desirable consistency. Preferred thickening agents are
carboxyvinyl polymers, carrageenan, hydroxyethyl cellulose, and
water soluble salts of cellulose ethers such as sodium
carboxymethylcellulose and sodium hydroxyethyl cellulose. Natural
gums such as gum karaya, xanthan gum, gum arabic, and gum
tragacanth can also be used. Colloidal magnesium aluminum silicate
or finely divided silica can be used as part of the thickening
agent to further improve texture. Thickening agents can be used in
an amount from about 0.1% to about 15%, by weight of the dentifrice
composition.
[0065] Water employed in the preparation of commercially suitable
oral compositions should preferably be of low ion content and free
of organic impurities. The dentifrice composition will contain a
water of from about 1% to about 20%, preferably from about 2% to
about 14%, and more preferably from about 3% to about 10%, by
weight of the composition. The amounts of water include the free
water which is added plus that which is introduced with other
materials, such as with sorbitol, silica, surfactant solutions,
and/or color solutions. Preferably, no free water is added to the
compositions herein. Without being limited by theory, it is
believed that the minimization of water in the compositions herein
reduces the negative interaction between polyphosphate and
fluoride, slows down polyphosphate hydrolysis, as well as
stabilizing stannous ion.
[0066] The present compositions may also comprise surfactants, also
commonly referred to as sudsing agents. Suitable surfactants are
those which are reasonably stable and foam throughout a wide pH
range. The surfactant may be anionic, nonionic, amphoteric,
zwitterionic, cationic, or mixtures thereof. Anionic surfactants
useful herein include the water-soluble salts of alkyl sulfates
having from 8 to 20 carbon atoms in the alkyl radical (e.g., sodium
alkyl sulfate) and the water-soluble salts of sulfonated
monoglycerides of fatty acids having from 8 to 20 carbon atoms.
Sodium lauryl sulfate and sodium coconut monoglyceride sulfonates
are examples of anionic surfactants of this type. Other suitable
anionic surfactants are sarcosinates, such as sodium lauroyl
sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauroyl
isethionate, sodium laureth carboxylate, and sodium dodecyl
benzenesulfonate. Mixtures of anionic surfactants can also be
employed. Many suitable anionic surfactants are disclosed by
Agricola et al., U.S. Pat. No. 3,959,458, issued May 25, 1976.
Nonionic surfactants which can be used in the compositions of the
present invention can be broadly defined as compounds produced by
the condensation of alkylene oxide groups (hydrophilic in nature)
with an organic hydrophobic compound which may be aliphatic or
alkyl--aromatic in nature. Examples of suitable nonionic
surfactants include poloxamers (sold under trade name Pluronic),
polyoxyethylene, polyoxyethylene sorbitan esters (sold under trade
name Tweens), fatty alcohol ethoxylates, polyethylene oxide
condensates of alkyl phenols, products derived from the
condensation of ethylene oxide with the reaction product of
propylene oxide and ethylene diamine, ethylene oxide condensates of
aliphatic alcohols, long chain tertiary amine oxides, long chain
tertiary phosphine oxides, long chain dialkyl sulfoxides, and
mixtures of such materials. The amphoteric surfactants useful in
the present invention can be broadly described as derivatives of
aliphatic secondary and tertiary amines in which the aliphatic
radical can be a straight chain or branched and wherein one of the
aliphatic substituents contains from about 8 to about 18 carbon
atoms and one contains an anionic water-solubilizing group, e.g.,
carboxylate, sulfonate, sulfate, phosphate, or phosphonate. Other
suitable amphoteric surfactants are betaines, specifically
cocamidopropyl betaine. Mixtures of amphoteric surfactants can also
be employed. Many of these suitable nonionic and amphoteric
surfactants are disclosed by Gieske et al., U.S. Pat. No.
4,051,234, issued Sep. 27, 1977. The present composition typically
comprises one or more surfactants each at a level of from about
0.25% to about 12%, preferably from about 0.5% to about 8%, and
most preferably from about 1% to about 6%, by weight of the
composition.
[0067] Titanium dioxide may also be added to the present
composition. Titanium dioxide is a white powder which adds opacity
to the compositions. Titanium dioxide generally comprises from
about 0.25% to about 5%, by weight of the composition. Similarly,
mica may added to the present compositions in order to provide
opacity and to further provide a shimmery or glittery appearance.
Mica generally comprises from about 0.1% to about 5%, by weight of
the composition.
[0068] Coloring agents may also be added to the present
composition. The coloring agent may be in the form of an aqueous
solution, preferably 1% coloring agent in a solution of water, or
in the form of pigments. Color solutions generally comprise from
about 0.01% to about 5%, by weight of the composition.
[0069] A flavor system can also be added to the compositions.
Suitable flavoring components include oil of wintergreen, oil of
peppermint, oil of spearmint, eucalyptus oil, clove bud oil,
menthol, anethole, methyl salicylate, eucalyptol, cassia, 1-menthyl
acetate, sage, eugenol, parsley oil, oxanone, alpha-irisone,
marjoram, lemon, orange, propenyl guaethol, cinnamon, vanillin,
ethyl vanillin, heliotropine, 4-cis-heptenal, diacetyl,
methyl-para-tert-butyl phenyl acetate, and mixtures thereof.
Coolants may also be part of the flavor system. Preferred coolants
in the present compositions are the paramenthan carboxyamide agents
such as N-ethyl-p-menthan-3-carboxamide (known commercially as
"WS-3") and mixtures thereof. A flavor system is generally used in
the compositions at levels of from about 0.001% to about 5%, by
weight of the composition.
[0070] The present invention may also include xylitol. Xylitol is a
sugar alcohol that is used as a sweetener and humectant. Xylitol
may provide a therapeutic effect, such as an antibacterial or
anticaries effect. The present compositions typically comprise
xylitol at a level from about 0.01% to about 25%, preferably from
about 3% to about 15%, more preferably from about 5% to about 12%,
and most preferably from about 9% to about 11%, by weight of the
total composition. Alternatively, if xylitol is used as a
sweetener, it may be present at a lower level, such as from about
0.005% to about 5%, by weight of the dentifrice composition.
[0071] Sweetening agents can be added to the compositions. These
include saccharin, dextrose, sucrose, lactose, maltose, levulose,
aspartame, sodium cyclamate, D-tryptophan, dihydrochalcones,
acesulfame, and mixtures thereof. Various coloring agents may also
be incorporated in the present invention. Sweetening agents and
coloring agents are generally used in toothpastes at levels of from
about 0.005% to about 5%, by weight of the composition.
[0072] The present invention may also include other agents, such as
antimicrobial agents. Included among such agents are water
insoluble non-cationic antimicrobial agents such as halogenated
diphenyl ethers, phenolic compounds including phenol and its
homologs, mono and poly-alkyl and aromatic halophenols, resorcinol
and its derivatives, bisphenolic compounds and halogenated
salicylanilides, benzoic esters, and halogenated carbanilides. The
water soluble antimicrobials include quaternary ammonium salts and
bis-biquanide salts, among others. Triclosan monophosphate is also
a suitable water soluble antimicrobial agent. The quaternary
ammonium agents include those in which one or two of the
substitutes on the quaternary nitrogen has a carbon chain length
(typically alkyl group) from about 8 to about 20, typically from
about 10 to about 18 carbon atoms while the remaining substitutes
(typically alkyl or benzyl group) have a lower number of carbon
atoms, such as from about 1 to about 7 carbon atoms, typically
methyl or ethyl groups. Dodecyl trimethyl ammonium bromide,
tetradecylpyridinium chloride, domiphen bromide,
N-tetradecyl-4-ethyl pyridinium chloride, dodecyl dimethyl
(2-phenoxyethyl) ammonium bromide, benzyl dimethylstearyl ammonium
chloride, cetyl pyridinium chloride, quaternized
5-amino-1,3-bis(2-ethyl-- hexyl)-5-methyl hexa hydropyrimidine,
benzalkonium chloride, benzethonium chloride and methyl
benzethonium chloride are exemplary of typical quaternary ammonium
antibacterial agents. Other compounds are
bis[4-(R-amino)-1-pyridinium] alkanes as disclosed in U.S. Pat. No.
4,206,215, issued Jun. 3, 1980, to Bailey. Stannous salts such as
stannous pyrophosphate and stannous gluconate and other
antimicrobials such as copper bisglycinate, copper glysinate, zinc
citrate, and zinc lactate may also be included. Also useful are
enzymes, including endoglycosidase, papain, dextranase, mutanase,
and mixtures thereof. Such agents are disclosed in U.S. Pat. No.
2,946,725, Jul. 26, 1960, to Norris et al. and in U.S. Pat. No.
4,051,234, Sep. 27, 1977 to Gieske et al. Specific antimicrobial
agents include chlorhexidine, triclosan, triclosan monophosphate,
and flavor oils such as thymol. Triclosan and other agents of this
type are disclosed in Parran, Jr. et al., U.S. Pat. No. 5,015,466,
issued May 14, 1991, and U.S. Pat. No. 4,894,220, Jan. 16, 1990 to
Nabi et al. These agents may be present at levels of from about
0.01% to about 1.5%, by weight of the composition.
[0073] Urea may also be present in the compositions herein. Without
being limited by theory, it is believed that urea acts as a
penetration agent to help the actives herein better diffuse into
the tooth enamel and/or the gum tissue. Urea may be present at
levels of from about 0.2% to about 5% by weight of the
composition.
[0074] A effective amount of a desensitizing agent may also be
incorporated in the compositions herein. The desensitizing agents
include those selected from alkaline metal salts with a chloride,
nitrate, sulfate, or acetate of a group ll metal or aluminum or
polymerizable monomer to occlude the tubules, alkaline metal or
ammonium oxylate, citric acid and sodium citrate. Preferred salts
are potassium nitrate, potassium citrate, and mixtures thereof.
Such desensitizing agents are disclosed in, e.g., U.S. Pat. No.
5,718,885, issued Feb. 17, 1998 to Gingold et al.
[0075] Method of Treatment
[0076] The present invention compositions additionally relate to a
method for reducing the incidence of calculus on dental enamel of a
human or animal, e.g., household pets or other domestic animals, or
animals kept in captivity. The method of treatment herein comprises
contacting the dental enamel surfaces in the mouth with the oral
compositions according to the present invention.
[0077] Examples & Method of Manufacturing
[0078] The following examples further describe and demonstrate
embodiments within the scope of the present invention. These
examples are given solely for the purpose of illustration and are
not to be construed as limitations of the present invention as many
variations thereof are possible without departing from the spirit
and scope.
EXAMPLES 1-6
[0079] The following examples are prepared according to the method
below.
1 Component Ex. 1 Ex. 2 Ex. 3 Ex. 4 Ex. 5 Ex. 6 Glass H 13 13 13 13
13 13 Polyphosphate Sodium 0.243 0.243 0.243 0.243 0.243 0.243
Fluoride Stannous 2.1 2.1 2.1 2.1 1.43 1.43 Chloride Dihydrate
Sodium Citrate 4 -- -- 4 -- 6 Sodium 2 -- -- 3 -- -- Dicarbonate
Sodium -- 0.8 -- -- -- 0.15 Hydroxide Tetrasodium -- -- 4 -- 4 --
Pyrophosphate Silica (Zeodent 21 21 21 21 21 23.322 119) Urea -- --
-- -- 1 -- Glycerin 27.451 29.451 29.251 29.451 29.451 29.451
PEG-300 6 7 9 7 8.47 7 Propylene 7 9 9 9 9 7 Glycol Xylitol 5 5 --
-- -- -- Poloxamer 3 3 3 3 3 3 Sodium Alkyl 2.09 2.09 2.09 2.09
2.09 2.09 Sulfate 27.9% Solution Mica 0.2 0.2 0.2 0.2 0.2 0.2
Acesulfame K -- 0.2 0.2 -- 0.2 0.2 Flavor 1.1 1.1 1.1 1.1 1.1 1.1
Saccharin 0.4 0.4 0.4 0.4 0.4 0.4 Blue Dye No. 1 0.006 0.006 0.006
0.006 0.006 0.004 D.I. Water 5.41 5.41 5.41 5.41 5.41 5.41 TOTAL
100 100 100 100 100 100
EXAMPLES 7-11
[0080] The following examples are prepared according to the method
below.
2 Component Ex. 7 Ex. 8 Ex. 9 Ex. 10 Ex. 11 Glass H Polyphosphate
13 13 -- 13 13 Sodaphos Polyphosphate -- -- 13 -- -- Sodium
Fluoride 0.243 0.243 0.243 0.243 0.243 Sodium -- -- -- -- --
Monofluorophosphate Stannous Chloride 1.43 1.43 1.43 1.43 1.43
Carboxymethycellulose 0.3 0.6 0.6 0.6 0.6 Water 5.41 5.41 5.41 5.41
5.41 Flavor 1.1 1.1 1.1 1.1 1.1 Glycerin 34.327 27.527 22.027 27.57
30.927 Poloxamer 407 6 3 5 5 3 Propylene Glycol 10 5 5 3 3 Sodium
Alkyl Sulfate 2.09 2.09 2.09 4 2.09 27.9% Solution Silica 10 22 20
17.547 27 Sodium Bicarbonate -- 15 15 15 5 Sodium Carbonate 2 2 2 2
2 Sodium Saccharin 0.4 0.5 0.4 0.4 0.5 Titanium Dioxide 0.5 0.5 0.5
0.5 0.5 Xanthan Gum 0.2 0.2 0.2 0.2 0.2 Polyethylene Glycol 12 -- 3
3 3 Calcium Peroxide 1 0.4 3 -- 1 TOTAL 100 100 100 100 100
EXAMPLES 12-16
[0081] The following examples are prepared according to the method
below.
3 Component Ex. 12 Ex. 13 Ex. 14 Ex. 15 Ex. 16 Glass H
Polyphosphate 13 13 -- 13 13 Sodaphos Polyphosphate -- -- 13 -- --
Sodium Fluoride -- -- -- -- -- Sodium 0.76 0.76 0.76 0.76 0.76
Monofluorophosphate Stannous Chloride 1.43 1.43 1.43 1.43 1.43
Carboxymethycellulose 0.6 0.6 0.6 0.6 0.6 Water 5.41 5.41 5.41 5.41
5.41 Flavor 1.1 1.1 1 1 1 Glycerin 25.44 25.44 25.44 40.51 25.01
Poloxamer 407 5 5 5 5 5 Propylene Glycol 3 3 3 3 3 Sodium Alkyl
Sulfate 2.09 2.09 2.09 2.09 4 27.9% Solution Silica 20.07 20.07
20.17 20 19.69 Sodium Bicarbonate 15 15 15 -- 15 Sodium Carbonate 2
2 2 2 2 Sodium Saccharin 0.4 0.4 0.4 0.5 0.4 Titanium Dioxide 0.5
0.5 0.5 0.5 0.5 Xanthan Gum 0.2 0.2 0.2 0.2 0.2 Polyethylene Glycol
3 3 3 3 3 Calcium Peroxide 1 1 1 1 -- TOTAL 100 100 100 100 100
[0082] The dentifrice compositions are prepared as follows. Add the
sodium alkyl sulfate solution, fluoride salts, sweeteners, and
coloring agents to the main mix tank. Agitate at the rate of
approximately 44.+-.4 rpm, and heat to about 40.+-.5.degree. C.
Maintain for about 20 minutes. Add about 1/3 of the glycerin to the
main mix tank, then add the poloxamer and homogenize for about 20
minutes. Add the remaining glycerin to the main mix tank. Add the
propylene glycol and PEG to a mixing vessel. In the main mix tank,
start agitator to pull a vortex for good mixing and homogenize for
5 minutes. Then decrease the temperature to approximately
35.degree. C. Add the silica to the main mix tank. After the
addition of the silica, completely open the vacuum to about 0.1 to
0.2 bar for 10 minutes. Add the flavor into the mixing vessel.
Premix the polyphosphate, the stannous salts, calcium peroxide (if
used) and sodium bicarbonate (if used), and the buffering agent,
then add into the main mix tank. Stir and homogenize for 20
minutes, then vacuum for 10 minutes at the end of the
homogenization.
[0083] It is understood that the examples and embodiments described
herein are for illustrative purposes only and that various
modifications or changes in light thereof will be suggested to one
skilled in the art without departing from the scope of the present
invention.
* * * * *